Trial results for Olpasiran in Chinese participants with elevated serum lipoprotein(a) were posted on ClinicalTrials.gov on 2025-02-10. The Phase 1 study evaluated the pharmacokinetic profile of single doses, showing a geometric mean maximum observed concentration (Cmax) of 144 ng/mL for the low dose group and 549 ng/mL for the high dose group.
Background
Elevated serum lipoprotein(a) (Lp[a]) is a recognized risk factor for cardiovascular disease. Understanding the pharmacokinetic profile of new therapies in diverse populations is crucial for their development.
Trial design
This completed Phase 1 study (NCT04987320) enrolled 24 Chinese participants with elevated serum lipoprotein(a). The main objective was to evaluate the pharmacokinetics of a single dose of Olpasiran in this specific population.
Key results
The study detailed several key pharmacokinetic parameters for Olpasiran:
- Maximum Observed Concentration (Cmax) of Olpasiran: The geometric mean Cmax was 144 ng/mL (Geometric Coefficient of Variation: 55.5%) for the low dose group and 549 ng/mL (Geometric Coefficient of Variation: 71.5%) for the high dose group.
- Area Under the Serum Concentration-time Curve From Time 0 Extrapolated to Infinity (AUCinf) of Olpasiran: The geometric mean AUCinf was 2660 h*ng/mL (Geometric Coefficient of Variation: 24.0%) for the low dose group and 12000 h*ng/mL (Geometric Coefficient of Variation: 41.2%) for the high dose group.
- Area Under the Serum Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) of Olpasiran: The geometric mean AUClast was 2660 h*ng/mL (Geometric Coefficient of Variation: 24.2%) for the low dose group and 12000 h*ng/mL (Geometric Coefficient of Variation: 41.3%) for the high dose group.
- Time to Cmax (Tmax) of Olpasiran: The median Tmax was 3.02 hours for the low dose group and 3.11 hours for the high dose group.
- Apparent Terminal Elimination Half-life (T1/2) of Olpasiran: The mean T1/2 was 6.05 hours (Standard Deviation: 1.59) for the low dose group and 6.69 hours (Standard Deviation: 1.58) for the high dose group.
- Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Olpasiran: The geometric mean Vz/F was 238 liters (Geometric Coefficient of Variation: 43.5%) for the low dose group and 176 liters (Geometric Coefficient of Variation: 60.2%) for the high dose group.
What this means
These pharmacokinetic results provide important data on how Olpasiran is absorbed, distributed, metabolized, and excreted in Chinese participants with elevated Lp(a). This information is foundational for understanding the drug's behavior in this specific population and will inform further clinical development, including dose selection for subsequent trials.
Source
The information regarding these trial results was obtained from ClinicalTrials.gov, a public database of clinical studies. The results for study NCT04987320, titled "A Study to Evaluate the Pharmacokinetics, Pharmacodynamics, Safety and Tolerability of Olpasiran in Chinese Participants With Elevated Serum Lipoprotein(a)," were posted on 2025-02-10 on clinicaltrials.gov.